title: [18F]fluoromethylbenzylsulfonate ester: a rapid and efficient synthetic method for the N-[18F]fluoromethylbenzylation of amides and amines.
abstract: We have prepared 4-[18F]fluoromethylbenzylsulfonate esters as fluoromethylbenzylating agents. These agents are readily prepared by an [18F]fluoride ion displacement of the corresponding bissulfonate esters. The application of these 4-[18F]fluoromethylbenzylsulfonate esters to N-alkylation reaction of spiperone and 1-phenylpiperazine shows that the products 3-N-(4-[18F]fluoromethylbenzyl)spiperone and 1-N-(4-[18F]fluoromethylbenzyl)-4-phenylpiperazine are rapidly produced with high radiochemical yields under a no-carrier-added condition.
authors.affiliation: Department of Nuclear Medicine, Samsung Medical Center, Seoul, South Korea.
authors.forename: Y S
authors.initials: YS
authors.lastname: Choe
authors.forename: D H
authors.initials: DH
authors.lastname: Song
authors.forename: K J
authors.initials: KJ
authors.lastname: Lee
authors.forename: S E
authors.initials: SE
authors.lastname: Kim
authors.forename: Y
authors.initials: Y
authors.lastname: Choi
authors.forename: K H
authors.initials: KH
authors.lastname: Lee
authors.forename: B T
authors.initials: BT
authors.lastname: Kim
authors.forename: S J
authors.initials: SJ
authors.lastname: Oh
authors.forename: D Y
authors.initials: DY
authors.lastname: Chi
mesh_terms: D000477:Alkylating Agents / Q000737:chemistry; D000478:Alkylation; D005462:Fluorine Radioisotopes / Q000737:chemistry*; D007553:Isotope Labeling / Q000379:methods*; D008698:Mesylates / Q000737:chemistry*; D010879:Piperazines / Q000737:chemistry; D013134:Spiperone / Q000737:chemistry
chemical_list: C110737:18F-fluoromethylbenzylsulfonate ester; D000477:Alkylating Agents; D005462:Fluorine Radioisotopes; D008698:Mesylates; D010879:Piperazines; D013134:Spiperone; C031503:phenylpiperazine